CATECHOL-O-METHYL TRANSFERASE INHIBITORS AND USE THEREOF IN TREATING PSYCHOTIC DISORDERS Russian patent published in 2016 - IPC C07D213/68 C07D401/10 C07D401/14 C07D405/08 C07D413/10 C07D413/14 C07D417/10 C07D417/12 C07D417/14 C07D413/06 A61K31/4412 A61K31/4427 A61K31/4709 A61P25/18 

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry, namely to derivatives of 4-pyridinone formula I or pharmaceutically acceptable salts thereof, where A is hydrogen, B(OH)₂, halogen, C(O)NH(CH₂)_nC(O)N(R³)₂; X is hydrogen or halogen; Y denotes phenyl, benzimidazolil, benztiazolil, benzoksazolil, benzpiperidinil, quinolyl, indolyl, indazolyl or pyridyl, each optionally substituted with 1-3 groups R^a, provided that Y denotes phenyl, then at least one of said R^a selected from OCF₃, O(CH₂)_nC_3-6cycloalkyl, NR²C(O)R², C(O)R², N(R²)₂, (CH₂)_nC(O)OR², OR², (CH₂)_nheterocyclyl, NH(CH₂)_nheterocyclyl, (CH₂)_n(C)_6-10aryl, O(CH₂)_nC_6-10aryl or O(CH₂)_nheterocyclyl, where said heterocyclic ring and aryl optionally substituted with 1-3 groups R^b; R¹ represents hydrogen, NR²R³, Si(CH₃)₃, (CH₂)_nC_6-10aryl, C₂alkenyl or C_1-4alkyl, said alkyl and alkenyl optionally substituted with 1-3 groups of halogen, OH, C_1-6alkyl, O-C_1-6alkyl, NR²R³, SOR², NHSO₂R², CF₃, C_6-10aryl, heterocyclyl, -C≡C-C_6-10aryl, C(O)NR²R³, wherein said aryl and heterocyclyl optionally substituted with 1-2 groups R^a; R² and R³ independently denote H, C_1-6alkyl, (CH₂)_nheterocyclyl, (CH₂)_nC_6-10aryl, wherein said aryl optionally substituted by group R^a or R² and R³ together with nitrogen atom to which they are bonded, form a 6-member ring, which contains oxygen; R^a is C_1-6alkyl, halogen, CF₃, OCF₃, C_3-6cycloalkyl, O(CH₂)_nC_3-6cycloalkyl, NR²C(O)R², C(O)R², CN, N(R²)₂, (CH₂)_nC(O)OR², OR², (CH₂)_nheterocyclyl, NH(CH₂)_nheterocyclyl, (CH₂)_nC_6-10aryl, O(CH₂)_nC_6-10aryl or O(CH₂)_nheterocyclyl, wherein said heterocyclyl and aryl optionally substituted with 1-3 groups R^b; R^b is C_1-6alkyl, halogen, CHF₂, oxo (=O), N(R²)₂, CH₂OH, S(O)₂NR²R³, (CH₂)_nC_6-10aryl, (CH₂)_nheterocyclyl, NH(CH₂)_nheterocyclyl, OR², C₃-₆cycloalkyl, CF₃ or CN; and n equals 0-3; and where heterocycle is aromatic or saturated or partially saturated monocyclic or bicyclic ring containing 5-10 atoms, among which 1-4 atoms are heteroatoms selected from nitrogen, oxygen and sulphur. Invention also relates to pharmaceutical composition based on compound of formula I, method of treating and/or preventing neurological and psychiatric disorders and method of intensifying action of antipsychotic agent based on use of compound of formula I.

EFFECT: new compounds are prepared effective in treating diseases associated with catechol-O-methyltransferase (COMT).

52 cl, 1 tbl, 17 ex